WO2001034587A3 - Process for preparing n-(4-hydroxy-phenyl)-n'-(4'-aminophenyl)-piperazine - Google Patents

Process for preparing n-(4-hydroxy-phenyl)-n'-(4'-aminophenyl)-piperazine Download PDF

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Publication number
WO2001034587A3
WO2001034587A3 PCT/US2000/030457 US0030457W WO0134587A3 WO 2001034587 A3 WO2001034587 A3 WO 2001034587A3 US 0030457 W US0030457 W US 0030457W WO 0134587 A3 WO0134587 A3 WO 0134587A3
Authority
WO
WIPO (PCT)
Prior art keywords
compound
formula
aminophenyl
piperazine
hydroxy
Prior art date
Application number
PCT/US2000/030457
Other languages
French (fr)
Other versions
WO2001034587A2 (en
Inventor
Brigitte Giesinger
Ingrid Mergelsberg
Original Assignee
Schering Corp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Schering Corp filed Critical Schering Corp
Priority to JP2001536534A priority Critical patent/JP4903963B2/en
Priority to EP00976949A priority patent/EP1230231B1/en
Priority to AT00976949T priority patent/ATE298325T1/en
Priority to AU14653/01A priority patent/AU1465301A/en
Priority to MXPA02004545A priority patent/MXPA02004545A/en
Priority to CA002390296A priority patent/CA2390296C/en
Priority to DE60020988T priority patent/DE60020988T2/en
Publication of WO2001034587A2 publication Critical patent/WO2001034587A2/en
Publication of WO2001034587A3 publication Critical patent/WO2001034587A3/en
Priority to HK02107791A priority patent/HK1046142A1/en

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/12Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
    • C07D295/135Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Cosmetics (AREA)

Abstract

A process is provided for producing a compound having formula: by (a) reacting a compound having formula (2.0) with a compound having formula (3.0) in the presence of an organic base selected from the group consisting of: triethylamine; N,N-diisopropylethylamine; 1,8-diazabicyclo[5.4.0]undec-7-ene (1,5-5); 1,5-diazabicyclo[4.3.0]non-5-ene; or 1,4-diazabicyclo[2.2.2]octane to form a compound having formula (4.0) ; and (b) reducing the compound of formula (4.0) to form the compound of formula (1.0), wherein X is Cl, Br, I or F.
PCT/US2000/030457 1999-11-08 2000-11-06 Process for preparing n-(4-hydroxy-phenyl)-n'-(4'-aminophenyl)-piperazine WO2001034587A2 (en)

Priority Applications (8)

Application Number Priority Date Filing Date Title
JP2001536534A JP4903963B2 (en) 1999-11-08 2000-11-06 Process for preparing N- (4-hydroxy-phenyl) -N '-(4'-aminophenyl) -piperazine
EP00976949A EP1230231B1 (en) 1999-11-08 2000-11-06 Process for preparing n-(4-hydroxyphenyl)-n'-(4'-aminophenyl)-piperazine
AT00976949T ATE298325T1 (en) 1999-11-08 2000-11-06 METHOD FOR PRODUCING N-(4-HYDROXYPHENYL)-N'-(4'-AMINOPHENYL)-PIPERAZ NE
AU14653/01A AU1465301A (en) 1999-11-08 2000-11-06 Process for preparing n-(4-hydroxy-phenyl)-n'-(4'-aminophenyl)-piperazine
MXPA02004545A MXPA02004545A (en) 1999-11-08 2000-11-06 Process for preparing n-(4-hydroxy-phenyl)-n -(4 -aminophenyl)-piperazine.
CA002390296A CA2390296C (en) 1999-11-08 2000-11-06 Process for preparing n-(4-hydroxy-phenyl)-n'-(4'-aminophenyl)-piperazine
DE60020988T DE60020988T2 (en) 1999-11-08 2000-11-06 METHOD OF PREPARING N- (4-HYDROXYPHENYL) -N '- (4'-AMINOPHENYL) -PIPERAZINE
HK02107791A HK1046142A1 (en) 1999-11-08 2002-10-28 Process for preparing n-(4hydroxyphenyl)-N' -4'-aminophenyl)- piperazine.

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US43504999A 1999-11-08 1999-11-08
US09/435,049 1999-11-08

Publications (2)

Publication Number Publication Date
WO2001034587A2 WO2001034587A2 (en) 2001-05-17
WO2001034587A3 true WO2001034587A3 (en) 2002-03-21

Family

ID=23726755

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2000/030457 WO2001034587A2 (en) 1999-11-08 2000-11-06 Process for preparing n-(4-hydroxy-phenyl)-n'-(4'-aminophenyl)-piperazine

Country Status (11)

Country Link
EP (1) EP1230231B1 (en)
JP (1) JP4903963B2 (en)
CN (1) CN1177840C (en)
AT (1) ATE298325T1 (en)
AU (1) AU1465301A (en)
CA (1) CA2390296C (en)
DE (1) DE60020988T2 (en)
ES (1) ES2240202T3 (en)
HK (1) HK1046142A1 (en)
MX (1) MXPA02004545A (en)
WO (1) WO2001034587A2 (en)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007075869A2 (en) 2005-12-23 2007-07-05 Ariad Pharmaceuticals, Inc. Bicyclic heteroaryl compounds
US9040539B2 (en) 2010-05-19 2015-05-26 Sandoz Ag Process for the preparation of chiral triazolones
RU2588570C2 (en) 2010-05-19 2016-07-10 Сандоз Аг Method of producing chiral hydrazides
BR112012029228A2 (en) 2010-05-19 2021-08-03 Sandoz Ag process for preparing a hydrogen chloride salt, hydrogen chloride salt, crystalline hydrogen chloride salt, using a salt and using the process
RU2580318C2 (en) 2010-05-19 2016-04-10 Сандоз Аг Obtaining intermediate products for synthesis of posaconazole
CN101824009A (en) * 2010-05-27 2010-09-08 北京德众万全药物技术开发有限公司 Simple preparation method for posaconazole and piperazine intermediate thereof
CN103635465A (en) 2011-06-16 2014-03-12 桑多斯股份公司 Process for the preparation of a chiral compound
CA3022250A1 (en) 2012-12-12 2014-06-12 Ariad Pharmaceuticals, Inc. Crystalline forms of 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-n-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide mono hydrochloride
EP2789610A1 (en) 2013-04-10 2014-10-15 Sandoz Ag Purification of Posaconazole Intermediates
CN108003118A (en) * 2017-12-27 2018-05-08 张家口市格瑞高新技术有限公司 A kind of posaconazole intermediate 1-(4- hydroxy phenyls)-4-(4- aminophenyls)The preparation process of-piperazine
CN114516849A (en) * 2020-11-18 2022-05-20 江苏恒盛药业有限公司 Synthesis method of 1- (4-aminophenyl) -4- (4-hydroxyphenyl) piperazine
CN114276315A (en) * 2021-12-16 2022-04-05 苏州汉德创宏生化科技有限公司 Preparation method of 4- [4- [4- (4-hydroxyphenyl) piperazine-1-yl ] phenyl carbamate

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0331232A2 (en) * 1988-02-29 1989-09-06 Janssen Pharmaceutica N.V. 5-lipoxygenase inhibiting 4-(4-phenyl-1-piperazinyl)phenols

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0753715B2 (en) * 1986-02-25 1995-06-07 大塚製薬株式会社 Benzoheterocyclic compound
JPH04247074A (en) * 1991-02-01 1992-09-03 Yoshitomi Pharmaceut Ind Ltd Production of 4-morpholinobenzoic acid derivative
DE4234295A1 (en) * 1992-10-12 1994-04-14 Thomae Gmbh Dr K Carboxylic acid derivatives, medicaments containing these compounds and process for their preparation
JPH0971564A (en) * 1995-07-06 1997-03-18 Japan Tobacco Inc Benzamidoxime derivative and its use in medicine

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0331232A2 (en) * 1988-02-29 1989-09-06 Janssen Pharmaceutica N.V. 5-lipoxygenase inhibiting 4-(4-phenyl-1-piperazinyl)phenols

Also Published As

Publication number Publication date
CN1177840C (en) 2004-12-01
DE60020988T2 (en) 2006-04-27
ES2240202T3 (en) 2005-10-16
WO2001034587A2 (en) 2001-05-17
AU1465301A (en) 2001-06-06
CA2390296C (en) 2009-12-29
JP2003513966A (en) 2003-04-15
HK1046142A1 (en) 2002-12-27
CN1387520A (en) 2002-12-25
ATE298325T1 (en) 2005-07-15
EP1230231A2 (en) 2002-08-14
EP1230231B1 (en) 2005-06-22
CA2390296A1 (en) 2001-05-17
MXPA02004545A (en) 2002-09-02
DE60020988D1 (en) 2005-07-28
JP4903963B2 (en) 2012-03-28

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